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目的:研究化合物告达庭口服给药后在大鼠体内的药代动力学过程。方法:大鼠单次灌胃给予告达庭后,于不同时间点采血以LC/ESI-MS/MS法检测血浆中药物浓度,并计算药代动力学参数。结果:大鼠分别单次口服10,20,40mg·kg-1剂量的告达庭后其半衰期分别为(1.59±1.08),(0.99±0.27),(1.92±1.55)h;AUC0-t分别为(220.6±114.8),(539.1±160.6),(1631.9±915.9)μg·h·L-1;cmax分别为(153.5±79.1),(232.8±119.3),(687.9±245.7)μg·L-1;tmax为(0.36±0.35),(1.33±0.61),(0.96±0.68)h。其AUC与给药剂量间呈现出非线性相关性。结论:在本实验所用剂量范围内告达庭在大鼠体内的动力学过程基本符合非线性动力学特征。
OBJECTIVE: To study the pharmacokinetics of compounds in rats after oral administration to rats. Methods: After a single intragastric administration to rats, the blood samples were collected at different time points and analyzed by LC / ESI-MS / MS. Pharmacokinetic parameters were calculated. Results: The half-lives of rats after single oral administration of 10,20,40 mg · kg-1 were (1.59 ± 1.08), (0.99 ± 0.27), (1.92 ± 1.55) h, respectively; AUC0-t Were (220.6 ± 114.8), (539.1 ± 160.6) and (1631.9 ± 915.9) μg · h · L-1, respectively. The values of cmax were (153.5 ± 79.1), (232.8 ± 119.3) and (687.9 ± 245.7) μg · L- 1; tmax was (0.36 ± 0.35), (1.33 ± 0.61), (0.96 ± 0.68) h. The AUC showed a non-linear correlation with the dose administered. CONCLUSION: The kinetics of glutamate in rats in the dose range used in this study is basically consistent with the nonlinear dynamics.